AZD4144 | AZD4144 : Inhibitor of NLRP3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Selectivity
Control Compounds
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
NLRP3
    • Ki:14 nM
    • IC50:76 nM
    • IC50:27 nM
    • IC50:25 nM
    Inhibitor
    up to 1 uM

    Selectivity

    Potency
    Cellular
    In Vitro

    NLRP3

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acs.jmedchem.5c00781

    In Vivo Validations

    Mouse
    Dose: 0.5 mg/Kg IV, 1 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Plasma half life: 4.0 ± 0.1 IV, 4.0 ± 0.4 PO h
    Systemic clearance: 0.87 ± 0.05 L/h/Kg
    Bioavailability: 53 ± 9%
    Volume of Distribution at Steady-State: 3.0 ± 0.1 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.5c00781

    Rat
    Dose: 0.5 IV, 1.0 PO mg/Kg
    Route of delivery: Intravenous, Oral
    Plasma half life: 2.9 ± 0.01 IV, 3.0 ± 0.01 h
    Systemic clearance: 0.38 ± 0.02 L/h/Kg
    Bioavailability: 79 ± 6%
    Volume of Distribution at Steady-State: 1.3 ± 0.01 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.5c00781

    Chemical Information

    Molecular Formula C18H16F3N3O3
    SMILEs OC[C@@H](O)CNc1nnc(-c2ccc(C(F)(F)F)cc2O)c2ccccc12
    InChI InChI=1S/C18H16F3N3O3/c19-18(20,21)10-5-6-14(15(27)7-10)16-12-3-1-2-4-13(12)17(24-23-16)22-8-11(26)9-25/h1-7,11,25-27H,8-9H2,(H,22,24)/t11-/m0/s1
    Molecular weight 379.11 Da
    AlogP 2.7863000000000007
    HBond acceptors 6
    HBond donors 4
    Atoms 43

    References

    Cross References

    canSARBindingDB

    Expert Reviews


    (on 4 Dec 2025 )
    Cellular Use Rating
    In Model Organisms
    Good cellular and in vivo tool compound for NLRP3. Additional activity data for rats, NLRP subfamily members, and a more general off target panel would be useful.
    (on 18 Dec 2025 )
    Cellular Use Rating
    In Model Organisms
    When using the compound in vivo, evaluate several concentrations within the range of 0.3 to 10 mg/kg since it is not possible to determine which dose allowed 50% inhibition based on data plotted in the...
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